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1. 发明授权

US07858785B2 Aminopyrimidine compounds and methods of use 有权
公开(公告)号：US07858785B2
公开(公告)日：2010-12-28
申请号：US12562853
申请日：2009-09-18
申请人： Adrian Leonard Smith , Paul Edward Brennan , Fenel F. Fils , Gang Liu , Nick A. Paras , Daniel Martin Retz , Elizabeth Rainbeau
发明人： Adrian Leonard Smith , Paul Edward Brennan , Fenel F. Fils , Gang Liu , Nick A. Paras , Daniel Martin Retz , Elizabeth Rainbeau
IPC分类号： C07D417/14 , A61K31/506 , A61P19/02 , A61P35/00
CPC分类号： C07D417/14 , C07D409/14
摘要： The invention relates to aminopyrimidine compounds useful for treating diseases mediated by polo-like kinase 1 (Plk1). The invention also relates to the therapeutic use of such aminopyrimidine compounds and compositions thereof in treating disease states associated with abnormal cell growth and unwanted cell proliferation.

2. 发明授权

US07786132B2 Aminopyrimidine compounds and methods of use 有权
标题翻译：氨基嘧啶化合物及其使用方法
公开(公告)号：US07786132B2
公开(公告)日：2010-08-31
申请号：US11304901
申请日：2005-12-16
申请人： Adrian Leonard Smith , Paul Edward Brennan , Frenel Fils DeMorin , Gang Liu , Nick A. Paras , Daniel Martin Retz , Elizabeth Rainbeau
发明人： Adrian Leonard Smith , Paul Edward Brennan , Frenel Fils DeMorin , Gang Liu , Nick A. Paras , Daniel Martin Retz , Elizabeth Rainbeau
IPC分类号： C07D409/14 , C07D417/14 , A61K31/506 , A61P19/02 , A61P35/00
CPC分类号： C07D417/14 , C07D409/14
摘要： The invention relates to aminopyrimidine compounds useful for treating diseases mediated by polo-like kinase 1 (Plk1). The invention also relates to the therapeutic use of such aminopyrimidine compounds and compositions thereof in treating disease states associated with abnormal cell growth and unwanted cell proliferation.
摘要翻译：本发明涉及可用于治疗由polo样激酶1（Plk1）介导的疾病的氨基嘧啶化合物。本发明还涉及这种氨基嘧啶化合物及其组合物在治疗与异常细胞生长和不想要的细胞增殖相关的疾病状态中的治疗用途。

3. 发明申请

US20100010014A1 AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE 有权
标题翻译：氨基嘧啶化合物和使用方法
公开(公告)号：US20100010014A1
公开(公告)日：2010-01-14
申请号：US12562853
申请日：2009-09-18
申请人： Adrian Leonard Smith , Paul Edward Brennan , Frenel Fils DeMorin , Gang Lin , Nick A. Paras , Daniel Martin Retz , Elizabeth Rainbeau
发明人： Adrian Leonard Smith , Paul Edward Brennan , Frenel Fils DeMorin , Gang Lin , Nick A. Paras , Daniel Martin Retz , Elizabeth Rainbeau
IPC分类号： A61K31/506 , C07D417/04 , C07D417/14 , A61P19/02 , A61P35/00
CPC分类号： C07D417/14 , C07D409/14
摘要： The invention relates to aminopyrimidine compounds useful for treating diseases mediated by polo-like kinase 1 (Plk1). The invention also relates to the therapeutic use of such aminopyrimidine compounds and compositions thereof in treating disease states associated with abnormal cell growth and unwanted cell proliferation.
摘要翻译：本发明涉及用于治疗由polo样激酶1（Plk1）介导的疾病的氨基嘧啶化合物。本发明还涉及这种氨基嘧啶化合物及其组合物在治疗与异常细胞生长和不想要的细胞增殖相关的疾病状态中的治疗用途。

4. 发明授权

US08440674B2 Substituted pyrimidine compounds as RAF inhibitors and methods of use 失效
标题翻译：取代的嘧啶化合物作为RAF抑制剂和使用方法
公开(公告)号：US08440674B2
公开(公告)日：2013-05-14
申请号：US13163666
申请日：2011-06-17
申请人： Frenel F. De Morin , Jian J. Chen , Elizabeth M. Doherty , Stephen A. Hitchcock , Qi Huang , Joseph L. Kim , Gang Liu , Thomas Nixey , Nick A. Paras , Jeffrey Petkus , Daniel Martin Retz , Adrian Leonard Smith , Jiawang Zhu
发明人： Frenel F. De Morin , Jian J. Chen , Elizabeth M. Doherty , Stephen A. Hitchcock , Qi Huang , Joseph L. Kim , Gang Liu , Thomas Nixey , Nick A. Paras , Jeffrey Petkus , Daniel Martin Retz , Adrian Leonard Smith , Jiawang Zhu
IPC分类号： A01N43/54
CPC分类号： C07D401/14 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein R1 is and A1, A2, A3, A4, X, Z, Z′, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译：本发明包括能够调节Raf激酶的新一类化合物，因此可用于治疗Raf激酶介导的疾病，包括黑素瘤，肿瘤和其它癌症相关病症。该化合物具有通式I，其中R1为和A1，A2，A3，A4，X，Z，Z'，R1，R2，R3，R4，R5和R6如本文所定义。本发明还包括药物组合物，用于治疗Raf激酶介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

5. 发明授权

US5721234A Glutamate receptor antagonists: fused cycloalkylouinoxalinediones 失效
标题翻译：谷氨酸受体拮抗剂：稠合的环烷氧基亚油酸盐
公开(公告)号：US5721234A
公开(公告)日：1998-02-24
申请号：US534526
申请日：1995-10-23
申请人： Christopher Franklin Bigge , Daniel Martin Retz
发明人： Christopher Franklin Bigge , Daniel Martin Retz
IPC分类号： C07C211/60 , C07C215/44 , C07C229/50 , C07C233/25 , C07C233/41 , C07C233/43 , C07C233/54 , C07C247/14 , C07C309/66 , C07D241/38 , A61K31/495 , C07D401/12 , C07D405/12
CPC分类号： C07D241/38 , C07C211/60 , C07C215/44 , C07C229/50 , C07C233/25 , C07C233/41 , C07C233/43 , C07C233/54 , C07C247/14 , C07C309/66 , C07C2102/10
摘要： Novel glutamate receptor antagonists represented by the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein Z is an alicyclic fused ring having 5 to 7 carbon atoms; R.sup.1 is hydrogen, an alkyl or an arylalkyl; and A is O, CH.sub.2, NR.sup.4, CH.sub.2 NR.sup.4, CN, tetrazole or CO wherein R.sup.4 is hydrogen, alkyl, hydroxyalkyl, aminoalkyl or aralkyl, wherein (i) when A is O, CH.sub.2, NR.sup.4 or CH.sub.2 NR.sup.4 then B is hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, hydroxyalkyl, alkoxy, aminoalkyl, heterocyclic, alkylheterocyclic, heterocyclic-methyl, heterocyclic-ethyl, alkylcarbonyl, cycloalkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclic-carbonyl, alkylheterocyclic-carbonyl, or when A is NR.sup.4 or CH.sub.2 NR.sup.4 then B is a naturally occurring .alpha.-amino acid moiety joined by an amide bond or B joins with R.sup.4 and the nitrogen to form a four to seven membered heterocyclic ring, provided that when Z is a fused cyclohexyl ring and R.sup.4 is hydrogen then B is not hydrogen; (ii) when A is CN then B is not present and Z is not a fused cyclohexyl ring; (iii) when A is tetrazole then B is hydrogen or alkyl having 1 to 6 carbon atoms; and (iv) when A is CO then B is hydroxy, alkoxy, aralkoxy, alkyl having 1 to 6 carbon atoms, aralkyl, NR.sup.7 R.sup.8.
摘要翻译：由式“IMAGE”表示的新型谷氨酸受体拮抗剂或其药学上可接受的盐，其中Z是具有5至7个碳原子的脂环稠合环; R1是氢，烷基或芳基烷基; 并且A是O，CH 2，NR 4，CH 2 NR 4，CN，四唑或CO，其中R 4是氢，烷基，羟基烷基，氨基烷基或芳烷基，其中（i）当A是O，CH 2，NR 4或CH 2 NR 4时，B是氢，烯基，炔基，芳基，芳烷基，羟基烷基，烷氧基，氨基烷基，杂环，烷基杂环，杂环 - 甲基，杂环 - 乙基，烷基羰基，环烷基羰基，芳基羰基，芳烷基羰基，杂环羰基，烷基杂环羰基，或当A为NR4或CH2NR4时 B是通过酰胺键连接的天然存在的α-氨基酸部分或B与R 4和氮连接形成4至7元杂环，条件是当Z为稠合环己基环且R 4为氢时，B不为氢; （ii）当A为CN时，B不存在，Z不为稠环己基环; （iii）当A是四唑时，B是氢或具有1至6个碳原子的烷基; 和（iv）当A是CO时，B是羟基，烷氧基，芳烷氧基，具有1至6个碳原子的烷基，芳烷基，NR 7 R 8。

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